Abstract: The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.

Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.

Abstract: The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.

Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.

Abstract: The present invention relates to certain salts of a 9E-15-(2-pyrrolidin-1-yl-ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5). 1(14,18)]hexacosa-1(24),2,4,9, 14,16,18(26),20,22-nonaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the citrate salt of this compound. The invention also relates to pharmaceutical compositions containing the citrate salt and methods of use of the citrate salt in the treatment of certain medical conditions.

Abstract: Compounds of the formula (I) are provided, including pharmaceutically acceptable salts thereof: which modulate ?-amyloid peptide (?-AP) production, and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.

Abstract: This invention relates to a stable pharmaceutical composition of freeze-dried tetrodotoxin powder which contains trace amount of tetrodotoxin, substances which can stabilizes tetrodotoxin, including disaccharide(s) or polyglucose(s) or analogues thereof and solvent(s), and solvents which can help tetrodotoxin dissolve.

Abstract: Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.

Abstract: The use of type V phosphodiesterase inhibitors as a novel independent therapeutic modality in the treatment of exercise induced pulmonary hemorrhage in equine is described. The type V phosphodiesterase inhibitor is injected into the horse intravenously as a stand-alone agent from about one-half hour to about seven (7) days prior to the onset of strenuous exercise.

Abstract: This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.

Abstract: The invention relates to novel heterocycles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.

Abstract: Provided are compounds of the formula: wherein RN1 is a substituent of formula G1-NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.

Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to heteroalkyl linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other conditions or disorders associated with kinases.

Abstract: The invention provides immunostimulatory compositions and methods of administration thereof. Also provided are methods of administering a tryptanthrin compound in an effective amount to enhance the immune response of a subject to an antigen. Also provided are methods of administering an effective amount of a tryptanthrin to stimulate the immune response in a subject for the treatment of cancer. Further provided are methods of administering a tryptanthrin compounds as an immunotherapeutic in the treatment of infectious diseases.

Abstract: A novel compound which is useful as an agent for treating and/or preventing emesis, vomiting and/or constipation. A compound represented by the formula (I): wherein R1 and R2 are each independently hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted cycloalkyl, optionally substituted aryl etc., R3 is hydrogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted lower alkoxy etc., R4 is hydrogen or lower alkyl, R5 is hydrogen, lower alkyl, cycloalkyl lower alkyl or lower alkenyl, or a pharmaceutically acceptably salt, or a solvate thereof is provided.

Abstract: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a):; R1 means a —(C?O)aOb(C1-C6)alkyl group, a —(C?O)aOb(C2-C6)alkenyl group, a —(C?O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C?O)aOb(C1-C6)alkyl group or a group of —(C?O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee 1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, R3 and R11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to heteroalkyl linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumors and cancers as well as other conditions or disorders associated with kinases.

Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.

Abstract: Compositions and methods of treating endothelial disorders, including: asthma, erectile dysfunction, pulmonary hypertension, cardiovascular disorders, and other disorders, using a synergistic combination of at least one arginase inhibitor and at least one phosphodiesterase (PDE1), (PDE2) and/or (PDE5) inhibitor are described.

Abstract: The present invention relates to novel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-? inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-? activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.

Abstract: The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment of psychosis, schizophrenia, schizoaffective disorder, schizophreniform disorder, psychotic disorder, delusional disorder, mania, or bipolar disorder.

Abstract: This invention relates to a stable pharmaceutical composition of freeze-dried tetrodotoxin powder which contains trace amount of tetrodotoxin, substances which can stabilizes tetrodotoxin, including disaccharide(s) or polyglucose(s) or analogues thereof and solvent(s), and solvents which can help tetrodotoxin dissolve.

Abstract: The present invention provides Wall Teichoic Acid biosynthesis inhibitors such as compound 1835F03 (targocil) and related synthetic analogs. The invention also provides pharmaceutical compositions thereof and methods for treating bacterial infection and the suppression of growth of bacterial cells by administering a Wall Teichoic Acid biosynthesis inhibitor. The invention is particularly useful for the treatment of Methicillin-resistant Staphylococcus aureus (MRSA). The invention further provides procedures for the syntheses of Wall Teichoic Acid biosynthesis inhibitors. The invention also provides methods for the identification of antibacterial therapeutic agents.

Abstract: The invention concerns a triterpene alkaloid of general formula (I). The invention also concerns a method for making same and use thereof as medicine.

Abstract: Compositions containing site 1 sodium channel blockers for use as local anesthetics with rapid nerve block, improved potency and efficacy, and no local toxicity have been developed. Liposomes were employed for increased loading of the site 1 sodium channel blocker, producing prolonged duration of block without systemic toxicity. In one embodiment, the compositions contain a site 1 sodium channel blocker alone. In another embodiment, the compositions contain a site 1 sodium channel blocker in combination with a corticosteroid. As demonstrated by the examples, encapsulating site 1 sodium channel blockers in liposomes results in rapid and prolonged nerve block without systemic toxicity, which is enhanced by the addition of a corticosteroid. Fluid liposomes showed more rapid release of STX than did solid ones, and dexamethasone accelerated STX release.

Abstract: The present invention describes tetracyclic compounds of formula (IA) or (IB), wherein the symbols R, X, A, Y, R2, R3 and D are as defined in the specification, their use in the treatment of certain diseases, e.g. depending on MK-2 or TNF activity, and ways of manufacturing them.

Abstract: Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4, R14, V, W, X, Y, Z, p, and ring A are as described in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

Abstract: O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described.

Abstract: [1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen atom attached at the 1- and/or 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.

Abstract: Compounds that inhibit phosphodiesterase 1 (PDE1) are useful to treat glaucoma or elevated intraocular pressure. The PDE1 inhibitors may be administered as monotherapy or in combination with additional intraocular-pressure lowering agents. In addition, the invention provides ophthalmic compositions comprising PDE 1 inhibitors and optionally one or more additional intraocular pressure-lowering agents. Topical and systemic therapy may be used.

Abstract: Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.

Abstract: The present invention relates to certain salts of a 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the citrate salt of this compound. The invention also relates to pharmaceutical compositions containing the citrate salt and methods of use of the citrate salt in the treatment of certain medical conditions.

Abstract: Compounds from 14 Kenyan plants, including from the root of Dovyalis abyssinica and Clutia robusta have been characterized and isolated, and their uses are disclosed.

Abstract: At least one active pharmaceutical ingredient is chosen from polycyclic quinazolines of formula V, pharmaceutically acceptable salts thereof, and hydrates of the pharmaceutically acceptable salts. The active pharmaceutical ingredients disclosed may be inhibitors of protein tyrosine kinase inhibitors and/or aurora kinase. The active pharmaceutical ingredients can be used for treating cancers susceptible to treatment with protein tyrosine kinase inhibitors and/or aurora kinase inhibitors.

Abstract: The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity.

Abstract: The present invention relates to certain salts of a 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26triaza-tetra-cyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the maleate salt of this compound. The invention also relates to pharmaceutical compositions containing this salt and methods of use of the salt in the treatment of certain medical conditions.

Abstract: The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.

Abstract: Optionally substituted 3-(thio, sulfonyl or sulfonyl)-7,8-dihydro-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one or a substituted 3-(thio, sulfinyl or sulfonyl)-7,8,9-trihydro-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.

Abstract: The present invention relates to compounds of Formula (I); to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.

Abstract: The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.

Abstract: Chemical permeation enhancers (CPEs) improve access of local anesthetics to the nerve, thereby improving their performance. Surfactants, representing three CPE sub-groups: anionic, cationic, and nonionic surfactants, were co-injected with tetrodotoxin (TTX) or bupivacaine at the sciatic nerve of Sprague-Dawley rats. All enhancers produced marked concentration-dependent improvements in the frequency and duration of block with TTX but not bupivacaine. An in vitro toxicity assay showed a wide range of CPE myotoxicity, but in vivo histological assessment showed no signs of muscle or nerve damage at concentrations of CPEs that produced a half-maximal increase in the duration of block of TTX. There was no systematic relationship between the enhancers' charge or hydrophobicity and their enhancement of block duration or potency.

Abstract: A cancer therapeutic agent comprising a combination of compound A described below, or a pharmaceutically acceptable salt thereof, and compound B described below, or a pharmaceutically acceptable salt thereof: Compound A represented by the formula of claim 1 and Compound B represented by: at least one type of compound selected from the group consisting of a platinum-type anticancer compound, selected from the group consisting of cisplatin carboplatin, oxaliplatin and nedaplatin; a gemcitabine-type compound, selected from the group consisting of gemcitabine and Ara-C; a 5-FU-type compound, selected from the group consisting of 5-FU, doxifluridine, UFT, carmofur, S-1, and capecitabine; a texane-type compound, selected from the group consisting of Taxol, Taxotere, IDN 5109, BMS 188797 BMS 184476 paclitaxel and docetaxel; a vinca alkaloid-type compound, selected from the group consisting of vinorelbine, vincristine, vinblastine, and videsine; an anticancer tyrosine kinase inhibitor compound, and an anticancer mo

Abstract: Compounds, compositions and methods are provided for treating malaria parasites in vitro and in vivo by administering indolo [2,1-b]quinazoline-6,12-dione compounds of Formula I.

Abstract: A stable freeze-dried powder preparation of tetrodotoxin and the producing method thereof. The freeze-dried powder preparation has tetrodotoxin as the main active ingredient, and comprises solubilizer, excipient and stabilizer. The said solubilizer is citric acid. The excipient is sodium chloride, mannitol or their composite. The stabilizer is dextran, trehalose or their composite. The ratio of tetrodotoxin, excipient and stabilizer is 1:150-3000:50-500 or 50-6000. Preferably, the preparation comprises lidocaine hydrochloride as function modulator. The preparation of the present invention can be used for avoiding the dependent abstinence syndrome of drugs such as opiates and cannabis.

Abstract: HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole, triazole, tetrazole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, and thiadiazole; R1 is halo, cyano, nitro, C1-6alkyl, polyhaloC1-6alkyl, —C1-6alkyl-OR4, —C(?O)—R5, —C(?O)—OR4, —C(?O)—NR6R7, —OR4, —O—C(?O)—C1-6alkyl, —O—C1-6alkyl-OR4, —O—C1-6alkyl-NR6R7, —O—C1-6alkyl-O—C(?O)—C1-6alkyl, —O—C1-6alkyl-C(?O)—OR4, —O—C1-6alkyl-C(?O)—NR6R7, —NR6R7, —NR8—C(?O)—R5, —NR8—C(?O)—OR4, —NR8—C(?O)—NR6R7, —NR8—C(?O)—C1-6alkyl-C(?O)—OR4, —NR8—C1-6alkyl-OR4, —NR8—C1-6alkyl-NR6R7, —NR8—C1-6alkyl-imidazolyl, —NR8—SO2R9, —N?CH—NR6R7, —NH—C(?NH)—NH2, —SO2NR6R7, and —O—PO(OR8)2; D forms pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, imidazole, pyrazole, furane, oxazole, isoxazole, thiophene, thiazole, and isothiazole; R2 is C1-6alkyl, polyhaloC1-6alkyl, halo, cyano, —COOR4, —OR4, and —NR6R7; R3 is phenyl, pyridyl, pyrimid

Abstract: Various agents are described to denerve, modulate, or otherwise affect the renal nerves and other neural tissue. Also, various delivery devices are described to deliver an agent locally to the renal nerves. The delivery devices are positioned in the renal artery and penetrate into the wall of the renal artery to deliver the agent to the renal nerves. The delivery devices may be used to deliver the agent according to longitudinal position, radial position, and depth of the renal nerves relative to the renal artery. In addition, various methods are described to denervate, modulate, or otherwise affect the renal nerves and other neural tissue.

Abstract: In one aspect, the present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to method for their preparation.

Abstract: The invention relates to novel heterocycles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.

Abstract: Compositions and methods are provided for the treatment of obesity in a human in need of such treatment which comprises administration to the human of a therapeutically effective amount of a compound of a weight loss enhancing beta-3-adrenergic compound of Cycle I, and a different weight loss enhancing adenylate cyclase receptor replenishing compound of Cycle II, in conjunction with a pharmaceutically acceptable diluent or carrier, wherein the Compound of Cycle I and the compound of Cycle II are administered sequentially. The composition may be present as a kit having each sequence in blister packs.